KR20210040064A - Ep4 수용체 길항제로서의 (r)-4-(1-(1-(4-(트리플루오로메틸)벤질)피롤리딘-2-카복스아미드)사이클로프로필 벤조산 - Google Patents

Ep4 수용체 길항제로서의 (r)-4-(1-(1-(4-(트리플루오로메틸)벤질)피롤리딘-2-카복스아미드)사이클로프로필 벤조산 Download PDF

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KR20210040064A
KR20210040064A KR1020217003353A KR20217003353A KR20210040064A KR 20210040064 A KR20210040064 A KR 20210040064A KR 1020217003353 A KR1020217003353 A KR 1020217003353A KR 20217003353 A KR20217003353 A KR 20217003353A KR 20210040064 A KR20210040064 A KR 20210040064A
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South Korea
Prior art keywords
compound
trifluoromethyl
benzyl
pyrrolidine
carboxamide
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KR1020217003353A
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English (en)
Korean (ko)
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사브리나 푸치
프란체스코 마코벡
루시오 클라우디오 로바티
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로타팜 바이오테크 에스.알.엘
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Publication of KR20210040064A publication Critical patent/KR20210040064A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/402—1-aryl substituted, e.g. piretanide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
KR1020217003353A 2018-07-12 2019-07-04 Ep4 수용체 길항제로서의 (r)-4-(1-(1-(4-(트리플루오로메틸)벤질)피롤리딘-2-카복스아미드)사이클로프로필 벤조산 KR20210040064A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IT102018000007134 2018-07-12
IT201800007134 2018-07-12
PCT/IB2019/055711 WO2020012305A1 (en) 2018-07-12 2019-07-04 (r)-4-(1-(1-(4-(trifluoromethyl)benzyl)pyrrolidine-2-carboxamide)cyclopropyl)-benzoic acid as ep4 receptor antagonist

Publications (1)

Publication Number Publication Date
KR20210040064A true KR20210040064A (ko) 2021-04-12

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Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020217003353A KR20210040064A (ko) 2018-07-12 2019-07-04 Ep4 수용체 길항제로서의 (r)-4-(1-(1-(4-(트리플루오로메틸)벤질)피롤리딘-2-카복스아미드)사이클로프로필 벤조산

Country Status (9)

Country Link
US (1) US11718582B2 (zh)
EP (1) EP3820842B1 (zh)
JP (1) JP2021524494A (zh)
KR (1) KR20210040064A (zh)
CN (1) CN112638871A (zh)
AU (1) AU2019300449A1 (zh)
CA (1) CA3105786A1 (zh)
ES (1) ES2948293T3 (zh)
WO (1) WO2020012305A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102394875B1 (ko) * 2021-05-11 2022-05-06 주식회사 비드테크 피롤리딘을 링커로 포함하는 화합물 및 이를 포함하는 약학 조성물

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3827828A1 (en) * 2019-11-29 2021-06-02 Rottapharm Biotech S.r.l. (r)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)-cyclopropyl) benzoic acid or its salt also in polymorphic form a for use in the prevention of heterotopic ossification
WO2022102731A1 (ja) 2020-11-13 2022-05-19 小野薬品工業株式会社 Ｅｐ４拮抗薬と免疫チェックポイント阻害物質との併用によるがん治療
CN113416162B (zh) * 2021-07-29 2023-02-10 南开大学 一种双手性联萘o-n-n三齿配体及其制备方法
WO2023223951A1 (ja) * 2022-05-16 2023-11-23 Ａｇｃ株式会社 ＩＬ－６及び／又はＩＬ－１β抑制剤

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2679175C (en) * 2007-02-26 2015-01-13 Merck Frosst Canada Ltd. Indole and indoline cyclopropyl amide derivatives as ep4 receptor antagonists
WO2010121382A1 (en) * 2009-04-21 2010-10-28 Merck Frosst Canada Ltd. Process for making indole cyclopropyl amide derivatives
US8828987B2 (en) * 2010-12-10 2014-09-09 Rottapharm Biotech S.R.L. Pyridine amide derivatives as EP4 receptor antagonists
WO2012103071A2 (en) * 2011-01-25 2012-08-02 Eisai R&D Management Co., Ltd. Compounds and compositions
BR112014000087B1 (pt) * 2011-07-04 2021-08-17 Rottapharm Biotech S.R.L. Derivados de amina cíclica como antagonistas do receptor ep4
EP2765128A1 (en) * 2013-02-07 2014-08-13 Almirall, S.A. Substituted benzamides with activity towards EP4 receptors

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102394875B1 (ko) * 2021-05-11 2022-05-06 주식회사 비드테크 피롤리딘을 링커로 포함하는 화합물 및 이를 포함하는 약학 조성물
WO2022239987A1 (ko) * 2021-05-11 2022-11-17 주식회사 비드테크 피롤리딘을 링커로 포함하는 화합물 및 이를 포함하는 약학 조성물

Also Published As

Publication number Publication date
WO2020012305A1 (en) 2020-01-16
ES2948293T3 (es) 2023-09-07
CN112638871A (zh) 2021-04-09
AU2019300449A1 (en) 2021-03-04
US11718582B2 (en) 2023-08-08
US20210130290A1 (en) 2021-05-06
CA3105786A1 (en) 2020-01-16
EP3820842B1 (en) 2023-03-29
EP3820842A1 (en) 2021-05-19
JP2021524494A (ja) 2021-09-13

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